• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    1511680 4 - Demethoxyadriomycin derivatives SOC FARMACEUTICI ITALIA SpA 15 Nov 1976 [18 Nov 1975] 47559/75 Heading C2C The invention comprises compounds (I) to (IV), where R 1 , R 2 and R 3 are H, Cl, Br, CH 3 or CH 3 O, provided that except when R 1 and R 3 are H and R 2 is CH 3 O, R 2 and R 3 are the same; R 4 is H or CF 3 CO and R 5 is OH, OCOR 6 (ocyloxy), OCOCH 2 OCOR 6 (alkenylglycollic ocyl) or NR 7 R 8 , where R 6 is C 6-16 hydrocarbyl and R 7 and R 8 are C alkyl or together with the nitrogen atom are 1-pyrrolidinyl, piperidins, morpholino or 4-methyl-1-piperozinyl. The compounds may be prepared by brominating a corresponding compound where R 5 is H and reacting the resulting bromo-compound with an appropriate sodium salt or an amine. The compounds of the invention have activity against malignant or transformed cell growth.
    公开号:SU727148A3
    申请号:SU762420456
    申请日:1976-11-17
    公开日:1980-04-05
    发明作者:Аркамоне Федерико；Бернарди Луиджи；Джардино Пьетро；Ди Марко Аурелио
    申请人:Сочиета Фармасьютичи Италиа С.П.А. (Фирма)；
    IPC主号:
    专利说明:

    This invention relates to a process for the preparation of new daunoaminyl anthracyclinone derivatives with antitumor activity. The purpose of the invention is to obtain new compounds expanding the range of means of action on a living organism. Based on the known reactions of broadening daunomycin derivatives and hydrolysis of the obtained J4-bromo derivatives using sodium formate 1, a method for the preparation of chloro-daunoamynyl anthracyclones of the general formula R, O OH o is proposed; - one where a / RI is hydrogen, identical, hydrogen, methyl, methoxy, chlorine or bromine, Rg and PZ are both hydrogen, hydrogen, methyl, NTE TOKCM, bromine, which is chlorine or total the compound OH OH (0), as defined above, is reserved in inert organic medium the solvent resulting from the 14-bromo derivative is subjected to hydrolysis by treatment with an aqueous solution of sodium formate and the resulting solution is held at 25 ° C, followed by treatment of the base obtained with hydrogen chloride. The desired product is isolated by known techniques. New compounds are characterized by the active suppression of the growth of malignant or transformed cells, in particular, they can be compared with well
    权利要求:
    Claims (1)
    [1]
    Claim
    A method of obtaining a daunoamininylanthracycline hydrochloride of the general Formula
    Ί
    - odi methoxy, where nacov, chlorine or
    b) K. g fight hydrogen, R methoxy, about t l
    L. V.,., Hydrogen ,, R, and hydrogen, methyl, bromine, and R both represent σόι ,,, ~ hydrogen, methyl, chlorine or bromine, and h a. · · и and с with the fact that the compound of the general formula
    I w, where the prisoners are 'above', k, oh he
    UT TO1 Gon to t U'yatt
    R, 0 · 0Η ’Λ4ί W but r
    R 4 , R and R 3 have the meanings, --------. - they are roasted in an inert organic solvent. the resulting 14-bromo derivative is subjected to hydrolysis by treatment with an aqueous solution of sodium formate and the resulting solution is maintained at 25 ° C, followed by treatment of the resulting base with hydrogen chloride.
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    SU727148A3|1980-04-05|Method of preparing daunoaminylanthracyclinones hydrochlorides
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    同族专利:
    公开号 | 公开日
    DK146542B|1983-10-31|
    CH625252A5|1981-09-15|
    JPS5736919B2|1982-08-06|
    AU1964376A|1978-05-25|
    MY8400400A|1984-12-31|
    DE2652391B2|1981-05-21|
    GB1511680A|1978-05-24|
    SE7612752L|1977-05-19|
    HK1282A|1982-01-22|
    CA1072546A|1980-02-26|
    DE2652391C3|1982-04-08|
    DK146542C|1984-04-09|
    NL178692B|1985-12-02|
    FR2347047B1|1980-03-14|
    BE848407A|1977-05-17|
    AT349633B|1979-04-10|
    ZA766851B|1978-06-28|
    AU499514B2|1979-04-26|
    ATA849076A|1978-09-15|
    DK513076A|1977-05-19|
    NL178692C|1986-05-01|
    NL7612389A|1977-05-23|
    FR2347047A1|1977-11-04|
    US4125607A|1978-11-14|
    DE2652391A1|1977-05-26|
    JPS5262269A|1977-05-23|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    DE2260438C3|1972-12-11|1980-01-10|Societa Farmaceutici Italia, Mailand |Adriamycin esters and their salts, processes for their preparation and pharmaceuticals|
    US4020270A|1974-05-02|1977-04-26|Societa' Farmaceutici Italia S.P.A.|L-lyxohex-1-enopyranose derivative|
    US4039663A|1975-03-19|1977-08-02|Societa' Farmaceutici Italia S.P.A.|Daunomycins, process for their uses and intermediates|
    GB1499026A|1975-06-20|1978-01-25|Farmaceutici Italia|Adriamycin esters|GB1535080A|1976-08-12|1978-12-06|Farmaceutici Italia|Naphthacenequinone derivatives|
    DE3100968A1|1980-01-16|1982-01-14|Farmitalia Carlo Erba S.p.A., 20159 Milano|Anthracycline derivatives, a process for their preparation and pharmaceuticals containing these compounds|
    US4585760A|1981-07-16|1986-04-29|American Cyanamid Company|Dimethylfurano heterocyclic analogs of daunomycin|
    JPS59212499A|1983-05-13|1984-12-01|Adoriya Lab Inc|4-demethoxy-3'-deamino-3' derivative|
    US4831019A|1983-10-31|1989-05-16|Adria Laboratories, Inc.|Pharmaceutical preparations of 4-demethoxy-n-trifluoroacetyl anthracyclines|
    JPS60188149A|1984-03-07|1985-09-25|Nakamatsu Yoshiro|Human body cooling apparatus|
    EP0183691A1|1984-06-14|1986-06-11|Biogal Gyogyszergyar|Process for preparing adriamycine and halide salts thereof|
    GB2169286A|1985-01-05|1986-07-09|Erba Farmitalia|4'-Deoxy-4'-halodoxorubicin-14-esters|
    GB2169285A|1985-01-05|1986-07-09|Erba Farmitalia|4'-Deoxydoxorubicin-14-esters|
    GB2169284A|1985-01-05|1986-07-09|Erba Farmitalia|4'-Epidoxorubicin-14-esters|
    US4663445A|1985-03-20|1987-05-05|The Ohio State Research Foundation|1-fluoro, 4-fluoro, and 1,4-difluoro-2'-halo anthracycline antibiotics|
    JPS6272356A|1985-09-25|1987-04-02|Matsushita Electric Works Ltd|Eye treatment device|
    KR0130906B1|1987-03-11|1998-04-23|팜이탈리아 카를로 에르바 에스. 알. 엘.|Immunoglobulin conjugates method and composition comprising|
    GB8708927D0|1987-04-14|1987-05-20|Erba Farmitalia|Chiral synthesis of anthracyclines|
    GB2212154B|1987-11-10|1991-03-27|Erba Carlo Spa|New 4-demethoxy anthracycline derivatives|
    US9828405B2|2013-04-29|2017-11-28|Nerviano Medical Sciences S.R.L.|Morpholinyl anthracycline derivatives|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    GB47559/75A|GB1511680A|1975-11-18|1975-11-18|Daunosaminyl anthracyclinones|
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